Synthesis and cytotoxic activities of 1-benzylidine substituted beta-carboline derivatives.
A series of new beta-carboline derivatives, bearing a benzylidine substituent at position-1, has been prepared and evaluated in vitro against a panel of human cell lines. The N(2)-benzylated beta-carbolinium bromates represented the most interesting cytotoxic activities. In particular, compounds 19 were found to be the most potent compounds with IC(50) values lower than 5 microM against 10 strains human tumor cell lines. These results confirmed that the N(2)-benzyl substituent on the beta-carboline ring played an important role in the modulation of the cytotoxic activities and suggested that further development of such compounds may be interest.
Cao
Rihui
R
School of Chemistry and Chemical Engineering, Sun Yat-sen (Zhongshan) University, 135 Xin Gang Xi Road, Guangzhou 510275, PR China. caorihui@mail.sysu.edu.cn
Yi
Wei
W
Wu
Qifeng
Q
Guan
Xiangdong
X
Feng
Manxiu
M
Ma
Chunming
C
Chen
Zhiyong
Z
Song
Huacan
H
Peng
Wenlie
W
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006247:Harmine / Q000138:chemical synthesis* / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D007477:Ions; D008956:Models, Chemical; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D002243:Carbolines; D007477:Ions; D006247:Harmine